Table of Content

25 December 2014, Volume 23 Issue 12

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Contents

Journal of Chinese Pharmaceutical Sciences

2014, 23(12):  811-814. 

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Review

Flavonoids: emerging trends and potential health benefits

Raj K. Keservani, Anil K. Sharma

2014, 23(12):  815-822.  DOI: 10.5246/jcps.2014.12.103

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Flavonoids are widely used in industry for the prevention of various diseases. In daily life we are directly in touch with flavonoids due to their presence in different beverages, fruits and vegetables. Flavonoids are mainly used as a coloring agent in plants, antioxidant and nutritional food for human. Flavonoids have explicit role in UV filtration, symbiotic nitrogen fixation and floral pigmentation. Flavonoids have potential for different biological activities like chelation of metals, decreasing platelets aggregation and cell signaling etc.



Original articles

Alginate-coated quaternized chitosan nanoparticles for oral delivery of insulin

Juan Bai, Jiancheng Wang

2014, 23(12):  823-829.  DOI: 10.5246/jcps.2014.12.104

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In the present work, we aimed to develop alginate-coated chitosan nanoparticles for oral insulin delivery. The N-[(2-hydroxy-3-trimethylammonium)propyl] chitosan chloride (HTCC) was synthesized, and the quaternized chitosan nanoparticles (HTCC-T NPs) were prepared by ionic gelation of HTCC using tripolyphosphate (TPP). The alginate-coated quaternized chitosan nanoparticles (HTCC-A NPs) were prepared by coating HTCC-T NPs with alginate (ALG) solution under mild agitation. Particle size, zeta potential, surface morphology, drug loading and entrapment efficiency of HTCC-A NPs were characterized using Zeta-sizer, TEM and HPLC assays. It was found that HTCC-A NPs exhibited uniform spherical particles with the size of (322.2±8.5) nm and positive charges (14.1±0.6) mV. Our data showed that the release behavior of HTCC-A NPs was quite different from that of HTCC-T NPs (without ALG coating) when incubated with various medium at different pH values in vitro, suggesting that ALG coating over the HTCC-T NPs improved the release profile of insulin from the NPs for a successful oral delivery. The ALG coatingcould also improve the stability of insulin against enzymatic degradation. From circular dichroism spectrum, it was revealed that HTCC-A NPs were capable of maintaining the conformation of insulin. The relative pharmacological bioavailability of HTCC-A NPs was 8.0%±2.5% by intraduodenal administration. The HTCC-A NPs significantly increased (P<0.05) the relative pharmacological availability (2.2 folds) compared with HTCC-T NPs after oral administration. HTCC-A NPs significantly enhanced the in vivo oral absorption of insulin and exhibited promising potentials for oral delivery.



Amavadin induced PTP opening not through the promotion of ROS generation in rat kidney mitochondria

Chenyi Huo, Huixue Liu

2014, 23(12):  830-836.  DOI: 10.5246/jcps.2014.12.105

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Amavadin is a natural vanadium compound that accumulates to high level in poisonous Amanita mushrooms. Recently, amavadin was found to have potential therapeutic effect in cancer treatment. However, its toxicity and the possible mechanism of actions are still not clear. In this study, we investigated the toxic effects of amavadin on rat kidney mitochondriaand the possible mechanism. We found that amavadin induced significantly permeability transition pore (PTP) opening in the mitochondria. Amavadin concentration-dependently inhibited the generation of reactiveoxygen species (ROS) in succinate buffer, and at high concentration of 200 μM it increased the ROS generation in malate buffer. With the addition of rotenone, the ROS generation in malate buffer was strongly enhanced than that induced by amavadin alone, but remained unchanged in succinate buffer. Results from the present study suggest that amavadin act upon electron transport chain downstream of rotenone, and the ubiquinone binding site in complex I is the most possible binding site.



Metformin activates Nrf2 signaling and induces the expression of antioxidant genes in skeletal muscle and C2C12 myoblasts

Simin Yang, Liyan Ji, Linling Que, Kui Wang, Siwang Yu

2014, 23(12):  837-843.  DOI: 10.5246/jcps.2014.12.106

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As a first line anti-diabetes drug, the molecular mechanisms by which metformin exerts its pharmacological activities are still under extensive investigations. The Nrf2 signaling plays a crucial role in protecting cells from oxidative damages, and has emerged as a promising target for treatment of diabetes and related complexes in recent years. In the present study, the effect of metformin on Nrf2 signaling was tested in vitro and in vivo, and the possible mechanism was explored. Metformin activated AMPK and Nrf2 signaling and induced the expression of antioxidant genes NQO1 and γ-GCSm in C2C12 mouse myoblast cells in a similar concentration- and time-dependent manner. Moreover, overexpression of AMPK significantly elevated the basal and metformin-induced ARE-driven luciferase reporter activities, suggesting the involvement of AMPK in metformin-activated Nrf2 signaling. Finally, metformin activated Nrf2 signaling and induced the expression of antioxidant genes such as HO-1 and SOD, and resulted in increased GSH level in mouse liver and skeletal muscle tissues. Take together, our results clearly demonstrated that metformin activated Nrf2 signaling and enhanced the tissue antioxidant capacity, and provide a new molecular mechanism of action of metformin.



Gastric ulcer healing effect of wild honey and its combination with Turmeric (Curcuma domestica Val.) Rhizome on male Wistar rats

I Ketut Adnyana, Joseph I. Sigit, Larasati A. Kusumawardani

2014, 23(12):  844-849.  DOI: 10.5246/jcps.2014.12.107

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Gastric ulcer is a common disorder in human at any ages. In this research, the antiulcer activity of wild honey produced by Apis dorsata, alone or in combination with Turmeric Rhizome, was evaluated in healing acute gastric ulcer. Male Wistar albino rats (150-250 g) were induced ulcers with aspirin at 405 mg/kg BW and ethanol. Antiulcer evaluation was done based on the gastric acidity, numbers and diameter of ulcers, ulcer index, healing ratio, histological examinations, and body weight. The results showed that the groups given honey alone, turmeric alone, and combination of turmeric-honey displayed significant ulcer healing compared to the control group. Ulcers in the group administered with combination of turmeric-wild honey was different significantly from the turmeric alone and wild honey alone groups with increased body weight in that group. The result showed that wild honey (2125 mg/kg BW) had the greatest activity in healing ulcers among other groups. The combination of turmeric-wild honey had a good activity in healing ulcers and increased the body weight of the group.



Investigation of the long-term stability and forced degradation of valtrate by high performance liquid chromatography coupled with triple quadrupole tandem mass spectrometry

Feifei Wang, Mingjuan Wang, Yumei Zhang, Yan Wang, Jiandong Yu, Ruizhong Wang, Xianlong Cheng, Qi Wang, Xiaowei Zheng, Yan Liu, Zhong Dai, Shuangcheng Ma, Erwin Adam

2014, 23(12):  850-857.  DOI: 10.5246/jcps.2014.12.108

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Valtrate is the main drug quality control for the qualitative and quantitative analysis of Valerian medicines in the Chinese Pharmacopoeia 2010.However, valtrate is unstable under some conditions. We, for the first time, systemically evaluated the stability of two bath reference standards (RS) by high performance liquid chromatography coupled with a triple quadrupole mass spectrometer(HPLC-MS/MS).The forced degradations of valtrate were performed to evaluate its optimal storage, transportation and experiment conditions according to ICH guideline.The developed HPLC method was validated to determine the degradation products. Valtrate RS was sensitive to alkaline and thermal conditions, but it was relatively stable under acidic, oxidation and photolysis conditions. A total of nine degradation components were identified under alkaline hydrolysis (N1–N4) andthermal degradation (B1–B5). The information obtained in this work would be valuable to minimize the decomposition of valtrate during the processes of preparation,storage, distribution and utilization. It was highly suggested to store valtrate with a single dose packing in brown closed ampoule at –20 ºC. Under the above-mentioned storage condition, valtrate could be stable for up to 3 years.



Synthesis, separation and NMR analysis of geometrical isomers of 3-benzylidene-indolin-2-one derivatives

Lingyu Li,Lunyong Shi, Hong Liang, Qingying Zhang

2014, 23(12):  858-865.  DOI: 10.5246/jcps.2014.12.109

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A series of E and Z-isomers of 3-(4'-substituted benzylidene)-indolin-2-one derivatives were synthesized and separated. Based on their ¹H NMR characterization, an unusual counterintuitive deshielding phenomenon for the protons presenting in the shielding zone of phenyl ring was observed and analyzed for the first time.



Simultaneous determination of four triterpenoid saponins and two liganoids in the roots of Ilex pubescens by RP-HPLC-DAD

Yuan Zhou, Ning Li, Jiayu Zhang, Yong Jiang, Pengfei Tu

2014, 23(12):  866-872.  DOI: 10.5246/jcps.2014.12.110

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A reversed-phase high performance liquid chromatography (RP-HPLC) method with diode array detector (DAD) has been established to simultaneously determine six bioactive compounds in the roots of Ilex pubescens, namely tortoside A, (+)-syringaresinol, ilexsaponin B₃, ilexsaponin A₁, ilexsaponin B₁, ilexgenin A. The RP-HPLC assay was performed on a reversed-phase C₁₈ column with a gradient elution. The mobile phase consisted of acetonitrile and water containing 0.1% (v/v) phosphoric acid. The flow rate was 1.0 mL/min and the detection wavelength was set at 210 nm. The six marker constituents were separated well with good linearity (r²>0.9996), precision, stability and repeatability. The overall recoveries were in the range of 99.00%–104.52%. Cluster analysis was employed to analyze 15 batches of samples. The result indicated this method provide an efficient way to perform quality control as well as a scientific rationale for the Geo-authentication of I. pubescens.



Short communication

Determination of the antioxidant activity based on the content changes in fatty acid methyl esters in vegetable oils

Housam Haj Hamdo, Zaid Al-Assaf, Warid Khayata

2014, 23(12):  873-877.  DOI: 10.5246/jcps.2014.12.111

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Free radicals, which are generated in several biochemical reactions in the body, have been implicated as mediators of many diseases, including cancer, atherosclerosis and heart diseases. Although the endogenous antioxidants can scavenge these free radicals, they are often insufficient to maintain the in vivo redox balance. The antioxidant activity (AOA) was examined by addition of each tested antioxidants [alpha-tocopherol (α-T), beta-tocopherol (β-T), gamma-tocopherol (γ-T), delta-tocopherol (δ-T), butylated hydroxyanisole (BHA), 2,6-di-tert-butyl-4-methylphenol (BHT), and ascorbyle palmitate (AP)] to four types of different vegetable oils (sunflower oil, soybean oil, corn oil and olive oil). Moreover, content changes in fatty acids were then investigated every 3 months during the storage period. The results showed that the AOA was different among the tested antioxidants. The AOA for BHA was the most for different types of oil compared with other antioxidants, whereas the δ-T possessed the lowest AOA.



Others

Contents of Volume 23

Journal of Chinese Pharmaceutical Sciences

2014, 23(12):  878-889. 

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Keywords Index of Volume 23

Journal of Chinese Pharmaceutical Sciences

2014, 23(12):  890-894. 

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Author Index of Volume 23

Journal of Chinese Pharmaceutical Sciences

2014, 23(12):  895-898. 

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Acknowledgements

Journal of Chinese Pharmaceutical Sciences

2014, 23(12):  899-899. 

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Journal of Chinese Pharmaceutical Sciences attended the 3rd Salon for Editors-in-chief of China Association for Science and Technology Sci-tech Journals

Journal of Chinese Pharmaceutical Sciences

2014, 23(12):  900-900. 

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The 3^rdSalon for editors-in-chiefof China Association for Science and Technology (CAST) sci-tech journals was held in Beijing on Nov 21^th, 2014. The theme of this Salon was “the mode of foreigner sci-tech journals in English”; “the internationalizationof China English sci-tech journals”; “how to improve the international influence of ChinaEnglish sci-tech journals”. Editors-in-chiefand presidents of CASTsci-tech journals gathered, discussing various topics of policy and development orientation of our sci-tech journals. Associate Prof. Heqing Huang, executive associate editor-in-chief of Journal of Chinese Pharmaceutical Sciences (JCPS) attended the Salon.